Reacción #674296

Ecuación de reacción

tert-Butyl 6-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)-2-azaspiro[3.3]heptane-2-carboxylate

Toluene

→

(±)-5-(1-(2-azaspiro[3.3]heptan-6-yl)-1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine formate

Rendimiento 61.0%

Disolventes

formic acid

Condiciones de reacción

Tratamiento posterior

1. 1
   OtroThe solution was sonicated at room temperature for 1.0 h
2. 2
   Concentraciónconcentrated by evaporation in vacuo
3. 3
   Otroto give the residue
4. 4
   Otroevaporated again
5. 5
   workup.ADDITIONEther (10 mL) was added
6. 6
   FiltraciónThe solid was collected by filtration
7. 7
   Lavadowashed with ether (10 mL)
8. 8
   Otrodried under high vacuum

Procedimiento

tert-Butyl 6-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)-2-azaspiro[3.3]heptane-2-carboxylate (53 mg, 0.094 mmol) was dissolved in formic acid (3 mL). The solution was sonicated at room temperature for 1.0 h and then concentrated by evaporation in vacuo to give the residue. Toluene (2×5 mL) was added and evaporated again. Ether (10 mL) was added and the mixture was stirred at room temperature for 1.0 h. The solid was collected by filtration, washed with ether (10 mL) and then dried under high vacuum to afford (±)-5-(1-(2-azaspiro[3.3]heptan-6-yl)-1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine formate (29 mg, 61%) as an off-white solid.

Fuente